Minnesota Eye Consultants, Minneapolis, Minnesota, USA.
J Ocul Pharmacol Ther. 2010 Dec;26(6):591-5. doi: 10.1089/jop.2010.0089. Epub 2010 Oct 6.
To compare the conjunctival concentrations of moxifloxacin after instillation of a single drop of moxifloxacin ophthalmic solution, 0.5% (Moxi) or a new 0.5% ophthalmic solution formulation (MAF) containing a retention-enhancing agent in patients undergoing cataract surgery.
This was a randomized, double-masked, parallel-group study. One hundred thirty patients scheduled for routine phacoemulsification and intraocular lens implantation were randomized to both treatment and post-dose sample collection time points. A single topical drop of Moxi or MAF was instilled in the study eye. At the designated time (0.25, 0.5, 1, 3, or 5 h post-dose), 2 conjunctival biopsy samples were obtained (N = 11-13 per treatment condition). Concentrations of moxifloxacin were determined using a validated ultra-performance liquid chromatography method. Moxifloxacin exposure [maximum mean moxifloxacin concentrations (C(max)) and area under the concentration-time curve (AUC)] was estimated from the observed concentration-time data.
The conjunctival moxifloxacin C(max), 43.8 μg/g, for MAF was achieved at 0.25 h. This was 1.8-fold higher than the C(max) for Moxi (24.1 μg/g), which was reached at 0.5 h post-dose. MAF AUC(0-3) was significantly greater than the AUC(0-3) of Moxi [50.5 (μg·h)/g vs. 27.1 (μg·h)/g; P < 0.05]. The conjunctival moxifloxacin C(max) for MAF was 337- to 730-fold greater than the reported minimum inhibitory concentration (MIC(90)) values for Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae. The C(max):MIC(90) ratios for Moxi ranged from 185 to 402. Conjunctival AUC(0-24):MIC(90) ratios ranged from 777 to 1,683 for MAF and from 625 to 1,355 for Moxi.
The new MAF ophthalmic formulation of moxifloxacin provided higher peak levels of moxifloxacin in the conjunctiva tissue, and larger total tissue exposure than the current, commercially available formulation. The superior penetration of MAF observed in this study could translate into greater eradication of bacteria.
比较白内障手术患者单滴 0.5%莫西沙星（Moxi）滴眼液或含有增效剂的新 0.5%滴眼液（MAF）后，结膜中莫西沙星的浓度。
这是一项随机、双盲、平行组研究。130 名接受常规超声乳化和人工晶状体植入术的患者被随机分配至两种治疗方案和给药后样本采集时间点。研究眼单滴 Moxi 或 MAF。在指定时间（给药后 0.25、0.5、1、3 或 5 小时），采集 2 个结膜活检样本（每种治疗条件下 11-13 个样本）。使用经过验证的超高效液相色谱法测定莫西沙星浓度。从观察到的浓度-时间数据中估算莫西沙星暴露量[最大平均莫西沙星浓度（C（max））和浓度-时间曲线下面积（AUC）]。
MAF 的结膜莫西沙星 C（max）为 43.8μg/g，在 0.25 小时达到。这是 Moxi（C（max）为 24.1μg/g）的 1.8 倍，后者在给药后 0.5 小时达到。MAF AUC（0-3）明显大于 Moxi AUC（0-3）[50.5（μg·h）/g 比 27.1（μg·h）/g；P<0.05]。MAF 的结膜莫西沙星 C（max）是金黄色葡萄球菌、肺炎链球菌和流感嗜血杆菌报告的最小抑菌浓度（MIC（90））值的 337-730 倍。Moxi 的 C（max）：MIC（90）比值范围为 185-402。MAF 的结膜 AUC（0-24）：MIC（90）比值范围为 777-1683，Moxi 的比值范围为 625-1355。
新型 MAF 莫西沙星滴眼液制剂在结膜组织中提供了更高的莫西沙星峰水平，并提供了比当前市售制剂更大的总组织暴露量。在这项研究中观察到的 MAF 更高的穿透性可能转化为更大的细菌清除率。
